EP2173354A4 - Chinoxalinderivate als pi3-kinase-inhibitoren - Google Patents
Chinoxalinderivate als pi3-kinase-inhibitorenInfo
- Publication number
- EP2173354A4 EP2173354A4 EP08797323A EP08797323A EP2173354A4 EP 2173354 A4 EP2173354 A4 EP 2173354A4 EP 08797323 A EP08797323 A EP 08797323A EP 08797323 A EP08797323 A EP 08797323A EP 2173354 A4 EP2173354 A4 EP 2173354A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- kinase inhibitors
- quinoxaline derivatives
- quinoxaline
- derivatives
- kinase
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 125000001567 quinoxalinyl group Chemical class N1=C(C=NC2=CC=CC=C12)* 0.000 title 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95484507P | 2007-08-09 | 2007-08-09 | |
| PCT/US2008/072401 WO2009021083A1 (en) | 2007-08-09 | 2008-08-07 | Quinoxaline derivatives as pi3 kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP2173354A1 EP2173354A1 (de) | 2010-04-14 |
| EP2173354A4 true EP2173354A4 (de) | 2011-10-05 |
Family
ID=40341726
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP08797323A Withdrawn EP2173354A4 (de) | 2007-08-09 | 2008-08-07 | Chinoxalinderivate als pi3-kinase-inhibitoren |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP2173354A4 (de) |
| JP (1) | JP2010535804A (de) |
| WO (1) | WO2009021083A1 (de) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0908905D0 (en) * | 2009-05-26 | 2009-07-01 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| JP5728683B2 (ja) * | 2009-09-04 | 2015-06-03 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン |
| GB201007286D0 (en) * | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) * | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| JP6166289B2 (ja) | 2012-03-14 | 2017-07-19 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 置換イミダゾピリダジン |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| LT3495367T (lt) | 2012-06-13 | 2021-02-25 | Incyte Holdings Corporation | Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| JP6193374B2 (ja) | 2012-08-13 | 2017-09-06 | 武田薬品工業株式会社 | Gpr6モジュレーターとしてのキノキサリン誘導体 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AU2014214326B2 (en) | 2013-02-07 | 2018-07-05 | Prexton Therapeutics Sa | Substituted quinoxaline derivatives and their use as positive allosteric modulators of mGluR4 |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| PE20160156A1 (es) | 2013-06-11 | 2016-04-20 | Bayer Pharma AG | Derivados de prodroga de triazolpiridinas sustituidas |
| WO2015059088A1 (de) * | 2013-10-23 | 2015-04-30 | Bayer Cropscience Ag | Substituierte chinoxalin-derivate als schädlingsbekämpfungsmittel |
| WO2015123505A1 (en) | 2014-02-14 | 2015-08-20 | Takeda Pharmaceutical Company Limited | Pyridopyrazines modulators of gpr6 |
| MA39784B1 (fr) | 2014-03-26 | 2021-03-31 | Astex Therapeutics Ltd | Combinaisons des inhibiteurs du fgfr et du cmet destinées au traitement du cancer |
| AU2015238305B2 (en) | 2014-03-26 | 2020-06-18 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| JO3695B1 (ar) | 2015-02-10 | 2020-08-27 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n- (3.5- ثنائي ميثوكسي فينيل)-n-(1-ميثيل إيثيل)-n- 3-( ميثيل-h1-بيرازول-4-يل) كينوكسالين-6-يل) إيثان- 1.2-ثنائي الأمين) |
| SG11201706287PA (en) | 2015-02-20 | 2017-09-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| KR20180030913A (ko) * | 2015-07-30 | 2018-03-26 | 브리스톨-마이어스 스큅 컴퍼니 | 아릴 치환된 비시클릭 헤테로아릴 화합물 |
| KR102703498B1 (ko) | 2015-09-23 | 2024-09-04 | 얀센 파마슈티카 엔브이 | 신규 화합물 |
| CN108137546B (zh) | 2015-09-23 | 2021-07-27 | 詹森药业有限公司 | 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途 |
| JP6912460B2 (ja) * | 2015-10-09 | 2021-08-04 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体 |
| US20190263804A1 (en) | 2016-06-16 | 2019-08-29 | Janssen Pharmaceutica Nv | Azabenzimidazole derivatives as pi3k beta inhibitors |
| KR102472453B1 (ko) | 2016-06-16 | 2022-11-29 | 얀센 파마슈티카 엔.브이. | Pi3k 베타 저해제로서의 이환식 피리딘, 피라진, 및 피리미딘 유도체 |
| EP3601254B1 (de) * | 2017-03-29 | 2022-05-25 | Janssen Pharmaceutica NV | Chinoxalin- und pyridopyrazinderivate als pi3k-beta-inhibitoren |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| ES3061844T3 (en) | 2018-05-04 | 2026-04-07 | Incyte Corp | Salts of an fgfr inhibitor |
| MX2020011718A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas. |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN112979613B (zh) * | 2019-12-16 | 2022-04-26 | 四川大学华西医院 | 2-(1h-吡唑-3-基)吡啶衍生物及其制备方法和用途 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| EP4352060A1 (de) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclische heterocyclen als fgfr-inhibitoren |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Fgfr阻害剤としての三環式ヘテロ環 |
| CN114605391B (zh) * | 2022-02-21 | 2024-01-26 | 广州六顺生物科技股份有限公司 | 喹喔啉类衍生物及其制备方法和应用 |
| WO2025160132A1 (en) * | 2024-01-23 | 2025-07-31 | Maplight Therapeutics, Inc. | Gpr6 inverse agonists |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1375486A1 (de) * | 2001-03-01 | 2004-01-02 | Shionogi & Co., Ltd. | Stickstoffhaltige heteroarylverbindungen mit hiv?integrase hemmender wirkung |
| US20040102360A1 (en) * | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
| WO2004050659A1 (en) * | 2002-11-27 | 2004-06-17 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| WO2008141065A1 (en) * | 2007-05-10 | 2008-11-20 | Smithkline Beecham Corporation | Quinoxaline derivatives as p13 kinase inhibitors |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006302179C1 (en) * | 2005-10-07 | 2013-06-20 | Exelixis, Inc. | N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
-
2008
- 2008-08-07 WO PCT/US2008/072401 patent/WO2009021083A1/en not_active Ceased
- 2008-08-07 JP JP2010520295A patent/JP2010535804A/ja not_active Withdrawn
- 2008-08-07 EP EP08797323A patent/EP2173354A4/de not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1375486A1 (de) * | 2001-03-01 | 2004-01-02 | Shionogi & Co., Ltd. | Stickstoffhaltige heteroarylverbindungen mit hiv?integrase hemmender wirkung |
| US20040102360A1 (en) * | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
| WO2004050659A1 (en) * | 2002-11-27 | 2004-06-17 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| WO2008141065A1 (en) * | 2007-05-10 | 2008-11-20 | Smithkline Beecham Corporation | Quinoxaline derivatives as p13 kinase inhibitors |
Non-Patent Citations (3)
| Title |
|---|
| FABIO ET AL.: "Antiamebic amidines and sulfonamides of 5- and 6-amino-2,3-bis(4-alkyl-1-piperazinyl)quinoxalines", J. MED. CHEM., vol. 23, no. 2, 1 January 1980 (1980-01-01), pages 201 - 206, XP002499777, DOI: 10.1021/JM00176A017 * |
| LINDSLEY ET AL.: "Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors", BIOORG. MED. CHEM. LETT., vol. 15, no. 3, 1 February 2005 (2005-02-01), pages 761 - 764, XP025314554, ISSN: 0960-894X, [retrieved on 20050201], DOI: 10.1016/J.BMCL.2004.11.011 * |
| See also references of WO2009021083A1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2173354A1 (de) | 2010-04-14 |
| WO2009021083A8 (en) | 2009-04-09 |
| WO2009021083A1 (en) | 2009-02-12 |
| JP2010535804A (ja) | 2010-11-25 |
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